BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases.
| Molecular Weight | 282.3 |
| Formula | C15H14N4O2 |
| CAS Number | 850717-64-5 |
| Solubility (25°C) | 27 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PDK1 Products |
|---|
| PDKtide
PDKtide is a biological active peptide. |
| PDK1-IN-RS2
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1. |
| PS47
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48. |
| PS210
PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
| WAY-299338
WAY-299338 is a modulator of the Protein Kinase PDK1. |
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